Fused heterocyclic compounds
    1.
    发明授权
    Fused heterocyclic compounds 失效
    稠合杂环化合物

    公开(公告)号:US07034039B2

    公开(公告)日:2006-04-25

    申请号:US10470805

    申请日:2002-02-01

    IPC分类号: C07D217/02 A61K31/47

    摘要: The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

    摘要翻译: 本发明提供下式的化合物:其中环A是任选取代的5至10元芳环; R 1和R 2相同或不同,并且各自为任选取代的烃基或任选取代的杂环基; X是一个键等; 和L是二价烃基及其盐,除了3-(氨基甲基)-2,6,7-三甲基-4-苯基-1(2H) - 异喹啉酮,3-(氨基甲基)-2-甲基-4 - 苯基-1(2H) - 异喹啉酮,3-(氨基甲基)-6-氯-2-甲基-4-苯基-1(2H) - 异喹啉酮和3-(氨基甲基)-2-异丙基-4-苯基-1 (2H) - 异喹啉酮。 该化合物显示出优异的肽酶抑制活性,并且可用作预防或治疗糖尿病等的药剂。

    Thienodipyridine derivatives, production and use thereof
    2.
    发明授权
    Thienodipyridine derivatives, production and use thereof 失效
    噻吩二吡啶衍生物,其生产和使用

    公开(公告)号:US06214838B1

    公开(公告)日:2001-04-10

    申请号:US09355218

    申请日:1999-07-23

    IPC分类号: A61K314365

    CPC分类号: C07D495/14

    摘要: A compound of the formula (I): wherein R is hydrogen or C2-6 alkanoyl; X is halogen; and ring A is benzene ring which is optionally substituted by 1 to 4 substituents selected from {circle around (1)} halogen, {circle around (2)} hydroxy, {circle around (3)} C1-6 alkoxy optionally substituted by halogen or phenyl, {circle around (4)} C1-6 alkylthio optionally substituted by halogen or phenyl, {circle around (5)} C1-6 alkyl optionally substituted by halogen, {circle around (6)} C2-6 alkanoylamino or {circle around (7)} carboxy optionally esterified by C1-6 alkyl, or a salt thereof; which can be used for preventing or treating inflammatory disease, arthritis, chronic rheumatoid arthritis, autoimmune diseases, or rejection after organ transplantation.

    摘要翻译: 式(I)的化合物:其中R是氢或C 2-6烷酰基; X是卤素; 并且环A是苯环,其任选被1至4个选自{(1)}周围的环,(2)}羟基周围的环,[(3)周围的环(任选被卤素取代)的C 1-6烷氧基 或苯基,(任选被(4)周围的环)被卤素或苯基任意取代的C 1-6烷硫基,((5)周围的环)任选被卤素取代的C 1-6烷基,(绕(6)周围的C 2-6烷酰基氨基或{ (7)}羧基,其任选被C 1-6烷基酯化,或其盐; 其可用于预防或治疗炎症性疾病,关节炎,慢性类风湿性关节炎,自身免疫性疾病或器官移植后的排斥反应。